健康志愿者单剂量毛冬青甲素的药代动力学研究及胶囊制剂的生物利用度  

Single-dose Pharmacokinetics of Ilexonin A in Healthy Subjects and the Bioavailability of Its Capsule

作　　者：王宁生[1] 刘启德[1] 邱卓嶷 丁有钦[2] 欧明[2] 周伟贞[3] 朱焯铨[3] 

机构地区：[1]广州中医学院临床药理研究所 [2]广州中医学院附属医院内科 [3]广州市医药工业研究所

出　　处：《广州中医学院学报》1989年第4期227-232,共6页

摘　　要：用高效液相色谱法测定了6名健康志愿者(4男2女)静注(20mg)和口服胶囊(120mg)毛冬青甲素后的血药浓度,用二房室药代动力学模型,分析了毛冬青甲素在体内的动力学过程.6名志愿者口服和静注的平均消除相常数和半衰期分别为0.0397 h^(-1),0.0460h^(-1)和17.7h,22.5h,体内总廓清率为4.6L/h。也用统计距分析法,求得口服毛冬青甲素的两个动力学参数MRT(体内平均滞留时间)和VRT(体内平均滞留时间的方差)分别为17.3h和1000 h^2,求得毛冬青甲素胶囊的绝对生物利用度为0.39。The pharmacokinetics of Ilexonin A and the bioavailability of its capsule were investigated. In the study six healthy subjects were administered with Ilexonin A both in a single oral dose (120mg) and i.v. dose (20mg) in a randomized cross- over trial. The unchanged drug level in plasma was measured by HPLC. The phar- macokinetic evaluation was based on assumption of an open two-compartment model. The elimination half-life(T1/2β) after oral and i.v. dosing were 17.7±2.4h and 22.5±2.9h respectively. The total clearance (Cl_(tot)) was 4.6±0.5L/h. The model-independent pharmacokinetic parameters MRT and VRT in oral administration were 17.3h and 1000h^2 respectively. The bioavailability of Ilexonin A capsule was 0.39 + 0.14 which was calculated by using the AUC. value corrected for intrai-ndividual variation in the elimination half-life and dose.

关 键 词：毛冬青甲素 药代动力学 生物效应 

分 类 号：R285.6[医药卫生—中药学]